Invention Grant
- Patent Title: Propane-1,3-dione derivative or salt thereof
- Patent Title (中): 丙烷-1,3-二酮衍生物或其盐
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Application No.: US11887384Application Date: 2006-03-30
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Publication No.: US07960562B2Publication Date: 2011-06-14
- Inventor: Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
- Applicant: Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
- Applicant Address: JP Tokyo
- Assignee: Astellas Pharma Inc.
- Current Assignee: Astellas Pharma Inc.
- Current Assignee Address: JP Tokyo
- Agency: Sughrue Mion, PLLC
- Priority: JPP.2005-101437 20050331; JPP.2005-353577 20051207
- International Application: PCT/JP2006/306641 WO 20060330
- International Announcement: WO2006/106812 WO 20061012
- Main IPC: A61K31/4184
- IPC: A61K31/4184 ; C07D235/12

Abstract:
It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
Public/Granted literature
- US20090181964A1 Propane-1,3-Dione Derivative or Salt Thereof Public/Granted day:2009-07-16
Information query
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